Acyclovir forte: instructions for use. Acyclovir forte tablets - instructions for use Acyclovir forte for what

S.01.A.D Antiviral drugs

- Treatment of skin and mucous membrane infections caused by virusesHerpes simplex types I and II,both primary and secondary, including genital herpes.

- Prevention of exacerbations of recurrent infections caused by virusesHerpes simplex types I and II, atpatients with normal immune status.

- Prevention of primary and recurrent infections caused by virusesHerpes simplex typelul atpatients with immunodeficiency.

- Treatment of primary and recurrent infections caused by the virusVaricella zoster(chickenpox, as well as herpes zoster -Herpes zoster).

List B.

In a dry place, protected from light, at a temperature not exceeding 25 ° C. Keep out of the reach of children.

2 years.

Do not use after expiration date.

Acyclovir forte: instructions for use and reviews

Release form

Pills

Compound

Acyclovir - 400 mg Excipients: potato starch, lactose (milk sugar), povidone, sugar (sucrose), sodium lauryl sulfate, magnesium stearate.

Pharmacological effect

An antiviral drug, a synthetic analogue of an acyclic purine nucleoside, which has a highly selective effect on herpes viruses. Inside virus-infected cells, under the influence of viral thymidine kinase, a series of sequential reactions of transformation of acyclovir into mono-, di- and triphosphate of acyclovir takes place. Acyclovir a triphosphate is integrated into the viral DNA chain and blocks its synthesis through competitive inhibition of viral DNA polymerase. In vitro, acyclovir is effective against the herpes simplex virus - Herpes simplex types I and II, against the Varicella zoster virus; higher concentrations are required to inhibit Epstein-Barr virus.

Pharmacokinetics

When taken orally, bioavailability is 15-30%. Acyclovir penetrates well into all organs and tissues of the body, including the brain and skin. Plasma protein binding is 9-33% and is independent of its plasma concentration. The concentration in the cerebrospinal fluid is about 50% of its concentration in plasma. Acyclovir crosses the placental barrier and accumulates in breast milk. The maximum concentration after oral administration of 200 mg 5 times a day is 0.7 mcg/ml, the time to reach the maximum concentration is 1.5-2 hours. Metabolized in the liver to form the pharmacologically inactive compound 9-carboxymethoxymethylguanine. The half-life in adults with normal renal function is 2-3 hours. In patients with severe renal failure, the half-life is 20 hours, with hemodialysis - 5.7 hours (at the same time, the concentration of acyclovir in plasma decreases to 60% of the initial value). About 84% is excreted by the kidneys unchanged and 14% in the form of a metabolite. The renal clearance of acyclovir is 75-80% of the total plasma clearance. Less than 2% of acyclovir is excreted from the body through the intestines.

Indications

Treatment of infections of the skin and mucous membranes caused by Herpes simplex viruses type I and II, both primary and secondary, including genital herpes. Prevention of exacerbations of recurrent infections caused by Herpes simplex viruses type I and II in patients with normal immune status. Prevention of primary and recurrent infections caused by Herpes simplex viruses type I and II in patients with immunodeficiency. As part of complex therapy for patients with severe immunodeficiency: with HIV infection (stage of AIDS, early clinical manifestations and detailed clinical picture) and in patients who have undergone bone marrow transplantation .Treatment of primary and recurrent infections caused by the Varicella zoster virus (chickenpox, as well as herpes zoster).

Contraindications

Hypersensitivity to acyclovir, ganciclovir or any excipient of the drug. Taking the drug is contraindicated during lactation. Children under 3 years of age (for this dosage form). Galactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Use during pregnancy and breastfeeding

Acyclovir crosses the placental barrier and accumulates in breast milk. Use during pregnancy is possible only if the expected benefit to the mother outweighs the potential risk to the fetus. If it is necessary to take acyclovir during lactation, interruption of breastfeeding is required.

Directions for use and doses

Inside. The drug is taken during or immediately after a meal and washed down with a sufficient amount of water. The dosage regimen is set individually depending on the severity of the disease. For the treatment of infections of the skin and mucous membranes caused by Herpes simplex types I and II: Adults: the drug is prescribed 200 mg 5 once a day for 5 days at 4-hour intervals during the day and at 8-hour intervals at night. In more severe cases of the disease, the course of treatment can be extended as prescribed by a doctor to 10 days. As part of complex therapy for severe immunodeficiency, including with a full-blown clinical picture of HIV infection (including early clinical manifestations of HIV infection and the stage of AIDS), after bone marrow implantation, 400 mg is prescribed 5 times a day. To prevent relapses of infections, caused by Herpessimplex viruses type I and II, patients with normal immune status and in case of relapse of the disease are prescribed 200 mg 4 times a day every 6 hours, course duration is from 6 to 12 months. For the prevention of infections caused by Herpessimplex viruses type I and II, adults with immunodeficiency, the drug is recommended to be prescribed 200 mg 4 times a day every 6 hours, the maximum dose is up to 400 mg of acyclovir 5 times a day, depending on the severity of the infection. Children: for infection caused by Herpes simplex and the prevention of this infection in patients with a weakened immune system protection, children over 3 years of age receive the same dose as adults. When treating infections caused by Varicella zoster: Adults: the drug is prescribed 800 mg 5 times a day every 4 hours during the day and at 8-hour intervals at night. The duration of the course of treatment is 7-10 days. Children: for chickenpox, 20 mg/kg is prescribed 4 times a day for 5 days (maximum single dose 800 mg), children from 3 years to 6 years: 400 mg 4 times a day, over 6 years: 800 mg 4 times a day for 5 days. When treating infections caused by Herpes zoster, adults are prescribed 800 mg 4 times a day every 6 hours for 5 days. In patients with impaired renal function: When treating and for the prevention of infections caused by Herpes simplex in patients with a creatinine clearance of less than 10 ml/min, the dosage of the drug should be reduced to 200 mg 2 times a day at 12-hour intervals. When treating infections caused by Varicella zoster in patients with a creatinine clearance of less than 10 ml/min it is recommended to reduce the dosage of the drug to 800 mg 2 times a day at 12-hour intervals; with creatinine clearance up to 25 ml/min, 800 mg is prescribed 3 times a day at 8-hour intervals.

Side effects

The drug is usually well tolerated. From the gastrointestinal tract: in isolated cases - abdominal pain, nausea, vomiting, diarrhea. In the blood: transient slight increase in the activity of liver enzymes, rarely - a slight increase in urea and creatinine levels, hyperbilirubinemia, leukopenia, erythropenia From the central nervous system: rarely - headache; weakness; in some cases, tremor, dizziness, increased fatigue, exhaustion, drowsiness, insomnia, paresthesia, confusion, hallucinations, decreased concentration, agitation. Allergic reactions: anaphylactic reactions, skin rash, itching, Lyell's syndrome, urticaria, exudative erythema multiforme, in incl. Stevens-Johnson syndrome, fever. Others: rarely - alopecia, peripheral edema, blurred vision, lymphadenopathy, myalgia, malaise.

Overdose

There have been no reported cases of overdose following oral administration of acyclovir.

Interaction with other drugs

Concomitant use with probenecid leads to an increase in the average half-life and a decrease in the clearance of acyclovir. When taken simultaneously with nephrotoxic drugs, the risk of renal dysfunction increases. An enhanced effect is observed with the simultaneous administration of immunostimulants.

special instructions

Use strictly as prescribed by a doctor to avoid complications in adults and children over 3 years of age. Prescribe with caution to patients with impaired renal function and elderly patients due to an increase in the half-life of acyclovir. When using the drug, it is necessary to ensure the intake of a sufficient amount of fluid. When taking of the drug, kidney function should be monitored (blood urea and plasma creatinine levels). Acyclovir does not prevent the sexual transmission of herpes, therefore, during the treatment period it is necessary to abstain from sexual intercourse, even in the absence of clinical manifestations. Due to the presence of lactose in the composition, patients with rare hereditary diseases such as galactose intolerance, lactase deficiency, glucose-galactose malabsorption should not take the drug.

"Acyclovir forte" is a drug with antiviral effects.

The drug has the following dosage form: tablets: biconvex, oblong, white, rounded ends, with a line on one side. In blister packs of five, ten, twelve, fifteen, twenty and thirty pieces, 1-3 packs per pack. The active substance of the tablet is acyclovir; sugar, magnesium stearate, potato starch, sodium lauryl sulfate, povidone, lactose are used as auxiliary components. "Acyclovir forte", the composition of which is described in detail in the instructions for the drug, can also be used for intravenous infusion.

Pharmacological properties

The drug "Acyclovir forte" is one of the antiviral drugs, synthetic analogues of purine acyclic nucleoside, which have a highly selective effect on herpes viruses. In cells infected with a virus, under the influence of viral thymidine kinase, sequential reactions are carried out converting acyclovir into di-, mono- and triphosphate of acyclovir. The drug effectively fights the herpes simplex virus - the first and second types of Herpes simplex, as well as the Varicella zoster virus; Higher concentrations are required to inhibit Epstein-Barr virus.

According to the instructions for use for Acyclovir Forte, the bioavailability of the active substance when taken orally ranges from 15 to 30 percent. Acyclovir penetrates perfectly into all organs and tissues of the human body, including the skin and brain. Binds to plasma proteins in the range of 9-33% (does not depend on plasma concentration). The concentration of the active substance in the cerebrospinal fluid is approximately 50% of the plasma concentration. Its maximum content after oral administration of 200 mg five times a day is 0.7 mcg/ml. It takes one and a half to two hours to reach maximum concentration.

The active component penetrates the placenta barrier and accumulates in a woman's milk. The result of metabolism is the formation in the liver of 9-carboxymethoxymethylguanine, a pharmacologically inactive compound. If the patient is an adult and his kidneys are functioning normally, then the half-life ranges from 2-3 hours.

Severe renal failure increases the half-life to twenty hours, 5-7 hours - with hemodialysis (the concentration of the active substance in plasma decreases to 60% of the initial value). About 84% of acyclovir is excreted by the kidneys in its original form, 14% - in the form of a metabolite. Clearance of the active substance by the kidneys is 75-80% of plasma clearance as a whole. Less than two percent of acyclovir is eliminated through the intestines.

In what cases is it used?

"Acyclovir forte" is used in the following cases:

• primary and secondary infections of the mucous membranes and/or skin caused by the first and second types of Herpes simplex viruses, including for the treatment of genital herpes;
• recurrent infections caused by viruses of the first and second types Herpes simplex with normal immunity status (as a prophylactic against exacerbations);
• recurrent and primary infections caused by viruses of the first and second types Herpes simplex with immunodeficiency (as a preventive measure);
• recurrent and primary infections caused by the Varicella zoster virus, including chickenpox and herpes zoster - Herpes zoster therapy;
• HIV infection (first clinical signs, stage of AIDS, detailed picture of the disease), patient’s condition after bone marrow transplantation (as part of complex therapy).

Contraindications

As the instructions for use for Acyclovir Forte indicate, absolute contraindications include: defects in the absorption of glucose and galactose, galactose intolerance, lactase deficiency; time of breastfeeding, patient age up to three years, as well as individual intolerance to one or another component of the drug and ganciclovir.

Relative contraindications, when the drug is prescribed under the supervision of a physician, are its use in large dosages, especially with dehydration; impaired renal function; neurological reactions and disorders when using cytotoxic drugs, including those with a complicated medical history; elderly age; pregnancy.

Dosage

Acyclovir forte 400 mg tablets should be taken orally with a sufficient amount of water, preferably immediately after or during a meal. It is used according to an individual scheme, based on the severity of the disease.

• Infections caused by the first and second types of the Herpes simplex virus: an antiviral drug is prescribed to adults five times a day (breaks of four hours during the day and eight at night are required) in a five-day course of 200 milligrams. Increasing the duration of the course to ten days becomes possible if the disease is severe. A single dosage of 400 milligrams is used for complex therapy of patients with severe immunodeficiency, including advanced clinical signs of HIV infection, as well as after bone marrow implantation. To prevent the recurrence of infections caused by Herpes simplex viruses, in case of relapse of the disease and the absence of defects in the immune status, Acyclovir Forte is prescribed four times a day (6-hour breaks) in a course of 6 to 12 months, 200 milligrams each. Adult patients with immunodeficiency are recommended to use the same dosages of the drug as prophylaxis. The maximum allowable dose is 400 milligrams five times a day (depending on the nature of the infection). "Acyclovir forte" for colds on the lips is prescribed to children in accordance with a regimen that is suitable for adults.

• Infections caused by Varicella zoster require the following dosages for adult patients: five times a day (with breaks during the day for four hours and at night for 8) 800 milligrams for 7-10 days; for chickenpox in children: 20 milligrams per kg four times a day (maximum 800 milligrams), five-day course; children from three to six years old - 400 milligrams four times a day; from six years - 800 milligrams four times a day. When treating Herpes zoster infections in adult patients, 800 milligrams are prescribed every six hours for a five-day course. The dosage of Acyclovir Forte must be strictly observed.
• What are the specifics of using Herpes simplex in patients with defects in kidney function? If creatinine clearance is less than 10 ml per minute, Acyclovir Forte is prescribed in a single dosage of 200 mg, twice a day (with twelve-hour breaks); Varicella zoster: with creatinine clearance, the drug is prescribed 800 mg, twice a day with the same breaks; if the clearance is from 10 to 25 ml per minute, the drug should be taken in the same single dosage three times a day with eight-hour breaks. Side effects of Acyclovir Forte tablets are generally well tolerated by patients.

An alternative may be the possibility of using Acyclovir in the form of intravenous infusions.

Side effects

When taking an antiviral drug orally, the following side effects may occur.

Immune system: in rare cases, anaphylaxis.

Digestive system: abdominal pain, diarrhea, vomiting and nausea; in rare cases - a transient increase in the activity of liver transaminases and bilirubin concentration; extremely rarely - jaundice and hepatitis.

CNS: dizziness and headache; in very rare cases - paresthesia, confusion, agitation, drowsiness, hallucinations, coma, encephalopathy, convulsions, dysarthria, ataxia, tremor, psychotic disorders.

Urinary system: in rare cases - a transient increase in the content of creatinine and urea in the blood plasma; very rarely - renal colic and acute kidney failure.

Respiratory system: in rare cases, shortness of breath may occur.

Subcutaneous tissues and skin: rash, including pruritus and photosensitivity, is common; infrequently - diffuse type hair loss (since this type of hair loss is caused by various pathologies and medications, the connection between it and the use of acyclovir is uncertain), urticaria; in rare cases - angioedema; even more rarely - exudative erythema multiforme, including Lyell and Stevens-Johnson syndromes.

Hematopoietic system: in very rare cases - thrombocytopenia, leukopenia and anemia.

Others: often - fatigue and fever; less often - malaise.

With intravenous infusions, the side effects are as follows.

Hematopoietic system: rarely - thrombocytopenia, leukopenia and anemia.

Immune system: in rare cases - anaphylaxis.

Digestive system: vomiting and nausea, much less often - abdominal pain and diarrhea.

Liver: quite often there is a transient increase in the activity of liver transaminases; very rarely - hepatitis, jaundice, transient increase in bilirubin concentration.

CNS: in rare cases - dizziness and headache, confusion, agitation, ataxia, tremor, hallucinations, dysarthria, psychotic signs, coma, encephalopathy, drowsiness and convulsions.

Often from the vascular system - phlebitis.

Organs of the mediastinum and chest, respiratory system: in very rare cases - shortness of breath.

Subcutaneous tissues and skin: often - rash, urticaria and itching (including photosensitivity); less often - angioedema.

Urinary system: often - increased concentrations of creatinine and urea in the blood; in very rare cases - impaired renal function, renal colic, acute kidney failure. The rapid increase in the degree of creatinine and urea in the blood is presumably due to the culmination of the content of acyclovir in the blood plasma, as well as the characteristics of water-salt metabolism.

To avoid such phenomena, intravenous infusion should be carried out slowly, over an hour. Colic in the kidney may be caused by defects in renal function. It is necessary to ensure the maintenance of normal water-salt metabolism in the human body. In rare cases, it can develop into acute renal failure.

General reactions: in rare cases - fever and general weakness.

Local reactions: the process of inflammation at the injection site. If acyclovir accidentally enters the space outside the cell, intravenous infusion may result in severe local inflammatory reactions, which can lead to destructive skin changes.

Use by pregnant and nursing mothers

During pregnancy, you can take Acyclovir Forte tablets only after assessing the risk-benefit ratio. You cannot take this drug while breastfeeding.

With defects in renal function and in old age

In accordance with the instructions, the drug is used with caution in case of impaired renal function. It is undesirable to use in case of serious defects in renal function. During administration, you need to monitor your condition (the level of urea in the blood, as well as creatinine in the blood plasma).

For elderly patients, “Acyclovir should be prescribed under the supervision of a specialist.

Special instructions for the use of the drug

It is necessary to take into account that when using Acyclovir Forte, acute kidney failure may develop due to the appearance of sediment from crystals of the active substance, which is especially possible with rapid intravenous administration, use along with nephrotoxic drugs, in patients with impaired renal function and with insufficient water load.

Not everyone knows what Acyclovir Forte helps with.

When using the drug, you need to monitor the condition of the kidneys (monitor the level of creatinine in the blood plasma and urea nitrogen in the blood).

Therapy in elderly patients should be carried out with a sufficient increase in fluid load and under medical supervision, since the half-life of acyclovir increases in this category.

During treatment for genital herpes, you should avoid intimate relationships or use condoms, because the use of the product does not prevent transmission of the virus to partners.

Analogues of "Acyclovir forte"

The medication has analogues such as Provirsan, Herperax, Acyclovir, Gervirax, Acigerpin, Zovirax, Medovir, Vivorax, Virolex. They must be prescribed by a doctor.

Zovirax in the form of a cream for external use is prescribed for the treatment of infections of the skin and mucous membranes caused by the herpes simplex virus types 1 and 2, including herpes labialis.

"Atsigerpin" - for herpes, prevents the formation of new rash elements, reduces the likelihood of skin dissemination and visceral complications, accelerates the formation of crusts, and reduces pain in the acute phase of herpes zoster. Has an immunostimulating effect.

tab. 400 mg: 10, 20 or 30 pcs. Reg. No.: LSR-007061/09

Clinical and pharmacological group:

Antiviral drug

Release form, composition and packaging

10 pieces. - contour cellular packaging (1) - cardboard packs.
10 pieces. - contour cell packaging (2) - cardboard packs.
10 pieces. - contour cell packaging (3) - cardboard packs.

Description of the active components of the drug " Acyclovir»

pharmachologic effect

Antiviral agent. Thymidine kinase in virus-infected cells actively converts acyclovir through a series of sequential reactions into acyclovir mono-, di- and triphosphate. The latter interacts with the viral DNA polymerase and is integrated into the DNA that is synthesized for new viruses. Thus, “defective” viral DNA is formed, which leads to suppression of the replication of new generations of viruses.

Acyclovir is active against Herpes simplex virus types 1 and 2, Varicella zoster virus, Epstein-Barr virus and cytomegalovirus.

Indications

For systemic use (orally and intravenously): infections caused by Herpes simplex viruses types 1 and 2 and Varicella zoster; prevention of infections caused by Herpes simplex and Varicella zoster viruses (including in patients with reduced immunity); as part of complex therapy for severe immunodeficiency (including the clinical picture of HIV infection) and in patients who have undergone bone marrow transplantation; prevention of cytomegalovirus infection after bone marrow transplantation.

For topical use in ophthalmology: keratitis and other eye lesions caused by the Herpes simplex virus.

For external use: skin infections caused by Herpes simplex and Varicella zoster viruses.

Dosage regimen

Orally for adults and children over 2 years old - 200-400 mg 3-5 times a day, if necessary - 20 mg/kg (up to 800 mg per dose) 4 times a day. In children under 2 years of age, use a dose equal to half the dose for adults. Duration of treatment is 5-10 days. In case of renal failure, adjustment of the dosage regimen is recommended.

IV drip for adults and children over 12 years old - 5-10 mg/kg, interval between injections - 8 hours. Children aged 3 months to 12 years - 250-500 mg/m 2 body surface, interval between injections - 8 hours. For newborns, the dose is 10 mg/kg, the interval between doses is 8 hours.

Apply locally and externally 5 times a day. The dose and duration of treatment depend on the indications and dosage form used.

Maximum doses: for adults with intravenous administration - 30 mg/kg/day.

Side effect

When taken orally: nausea, vomiting, diarrhea, abdominal pain, skin rash, headache, dizziness, fatigue, decreased concentration, hallucinations, drowsiness or insomnia, fever; rarely - hair loss, transient increase in blood concentrations of bilirubin, urea, creatinine, liver enzyme activity, lymphocytopenia, erythropenia, leukopenia.

With intravenous administration: acute renal failure, crystalluria, encephalopathy (confusion, hallucinations, agitation, tremor, convulsions, psychosis, drowsiness, coma), phlebitis or inflammation at the injection site, nausea, vomiting.

For local use: burning sensation at the application site, superficial punctate keratitis, blepharitis, conjunctivitis.

For external use: at the site of application, a burning sensation, skin rash, itching, peeling, erythema, dry skin are possible; upon contact with mucous membranes - inflammation.

Contraindications

Hypersensitivity to acyclovir and valacyclovir; with intravenous administration - lactation (breastfeeding).

Pregnancy and lactation

The use of acyclovir during pregnancy is possible in cases where the expected benefit to the mother outweighs the potential risk to the fetus.

IV use of acyclovir during lactation is contraindicated (excreted in breast milk).

IN experimental studies Animal studies have shown that acyclovir penetrates the placental barrier.

Use for renal impairment

In case of renal failure, adjustment of the dosage regimen is necessary.

Use in old age

Application for children

Orally for children over 2 years old - 200-400 mg 3-5 times a day, if necessary - 20 mg/kg (up to 800 mg per dose) 4 times a day. In children under 2 years of age, use a dose equal to half the dose for adults. Duration of treatment is 5-10 days.

special instructions

It should be taken into account that when using acyclovir, acute renal failure may develop due to the formation of sediment from acyclovir crystals, which is especially likely with rapid intravenous administration, simultaneous use of nephrotoxic drugs, in patients with impaired renal function and with insufficient water load.

When using acyclovir, it is necessary to monitor renal function (determining the level of urea nitrogen in the blood and creatinine in the blood plasma).

Treatment of elderly patients should be carried out with a sufficient increase in water load and under the supervision of a physician, because in this category of patients, the half-life of acyclovir increases.

When treating genital herpes, you should avoid sexual intercourse or use condoms, because the use of acyclovir does not prevent transmission of the virus to partners.

Acyclovir in the form of dosage forms for external use should not be applied to the mucous membranes of the mouth, eyes, or vagina.

Drug interactions

Drug interactions

With simultaneous use, probenecid reduces the tubular secretion of acyclovir and thereby increases the plasma concentration and half-life of acyclovir.

With the simultaneous use of acyclovir with nephrotoxic drugs, the risk of developing nephrotoxicity increases (especially in patients with impaired renal function).

An increase in the effect of acyclovir is observed with the simultaneous administration of immunostimulants.

When mixing solutions, it is necessary to take into account the alkaline reaction of acyclovir for intravenous administration (pH 11).